JP2007246429A - Lipase inhibitor, and food and drink - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide lipase activity inhibiting foods and drinks and an inhibitor, having excellent lipase activity inhibiting action and useful for obesity dissolution and/or suppression and/or prevention. <P>SOLUTION: The lipase activity inhibiting foods and drinks containing extracts of one or more plants selected from Glirichidia sepium (Jacq.) Walp, Adenanthera pavonina, Citrus hystrix, Michelia alba, Gustavia gracillima, Phyllanthus acidus, and Thunbergia laurifolia are provided. The lipase activity inhibitor contains the extracts of the plants as an active ingredient. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to a lipase activity-inhibiting food and drink and inhibitor that effectively inhibits the activity of lipase responsible for digestion and absorption of lipids in vivo and is useful for the elimination, suppression, and prevention of obesity.

In recent years, simple obesity due to westernization of meals and lack of exercise is increasing in Japan. Obesity is a major cause of various lifestyle-related diseases such as hypertension, diabetes and hyperlipidemia, and various diseases caused by arteriosclerosis.
Dietary lipids are absorbed into the small intestine by breaking down triacylglycerol, which occupies most of the lipid, into monoacylglycerol and free fatty acids by lipase in pancreatic juice. Therefore, it is considered that by inhibiting this lipase activity, absorption of diet-derived lipids can be suppressed, and obesity can be eliminated / suppressed / prevented.

In addition, triacylglycerol is mostly transported throughout the body as a component of lipoproteins in the blood and is hydrolyzed by the action of lipoprotein lipase that is mainly biosynthesized in muscle and adipose tissue and present on the inner wall of blood vessels. . That is, lipoprotein lipase is extremely important for the degradation of triacylglycerol in blood, and activating this enzyme is thought to lead to blood clarification.
Therefore, if the inhibition of lipase activity and the promotion of lipoprotein metabolism in blood can suppress lipid absorption and increase lipid metabolism in blood, not only obesity but also hyperlipidemia Expected to improve.

From such a viewpoint, the search of the natural origin component which has a lipase activity inhibitory effect is energetically performed. So far, banaba tea, yacon tea, gymnema, royal jelly, bittern and the like have been reported as having lipase activity inhibitory activity (see Patent Documents 1 and 2). In addition, dextran sulfate and the like have been reported as a component that enhances lipoprotein lipase activity.
However, the reality is that sufficient obesity elimination / suppression / prevention effects have not yet been obtained.
JP 2001-299272 A JP 2001-226274 A

  The present invention has been made in view of such circumstances, and it is an object to provide a lipase activity-inhibiting food and drink and an inhibitor that have an excellent lipase activity inhibitory action and are useful for the elimination, suppression, and prevention of obesity. And

  In order to solve the above-mentioned problems, the present inventor has eagerly searched for a substance having a lipase activity inhibitory action in natural products, and found that an extract extracted from a specific plant has an excellent lipase activity inhibitory action. It was. And when further examined, among the specific plants, an extract extracted from the bark of Madr lilac (Glirichidia sepium (Jacq.) Walp) inhibits lipase activity and enhances lipoprotein lipase activity, The present invention was completed by finding that it promotes lipoprotein metabolism in blood.

  That is, the present invention relates to the followings: Glirichidia sepium (Jacq.) Walp, Adenanthera pavonina, Citrus hystrix, Michelia alba, Gustavia gracillima, Phyllanthus acid And the said subject is solved by the food / beverage products for lipase activity inhibition characterized by containing the extract of the 1 type (s) or 2 or more types of plant chosen from Laurel Kazura (Thunbergia laurifolia).

  In addition, the present invention provides the above-mentioned problem by a food for reducing blood triglyceride, characterized by containing an extract obtained by extracting bark of madir lilac (Glirichidia sepium (Jacq.) Walp) with a polar solvent. It has been solved.

  In addition, the present invention relates to the following: And an lipase activity inhibitor characterized by containing an extract of one or more plants selected from Thunbergia laurifolia as an active ingredient.

  The present invention further provides a blood triglyceride-lowering agent characterized by comprising, as an active ingredient, an extract obtained by extracting bark of madril lilac (Glirichidia sepium (Jacq.) Walp) with a polar solvent. It has been solved.

  According to the lipase activity-inhibiting food and drink and the lipase activity inhibitor of the present invention, absorption of lipids into the body can be suppressed, and accordingly, the onset of obesity and various lifestyle-related diseases derived therefrom is prevented. be able to. Moreover, since the specific plant used for this invention is derived from nature, it is highly safe and can mix | blend in food-drinks and can also be continuously ingested. In particular, an extract derived from the bark of Glirichidia sepium (Jacq.) Walp among certain plants inhibits lipase activity, activates lipoprotein lipase, and promotes lipoprotein metabolism. ADVANTAGE OF THE INVENTION According to invention, the food-drinks and pharmaceutical which can further reduce the triglyceride in blood can be provided.

Plants used in the present invention are the following: lilac (Glirichidia sepium (Jacq.) Walp), Adenanthera pavonina, Citrus hystrix, Michelia alba, Gustavia gracillima, Phyllanthus acidus) and Thunbergia laurifolia. These plants are a kind of tropical plants that mainly live in the Kingdom of Thailand.
The extract of the present invention is obtained by extracting the above plant with a polar solvent as it is or after pretreatment such as drying, cutting, pulverization, and pulverization as necessary. In the extraction, any part of the plant can be used, but the bark or leaves of the plant is preferably used. In particular, it is preferable to use bark for mud lilac (Glirichidia sepium (Jacq.) Walp), and it is preferable to use leaves for other plants. These plants can be used alone or in combination of two or more.

  In the present invention, the polar solvent used for the extraction treatment includes an aqueous solvent or a hydrophilic organic solvent. Examples of the aqueous solvent include water, hot water, and physiological saline. Examples of the hydrophilic organic solvent include lower alcohols such as methanol, ethanol, propanol and butanol; esters such as ethyl acetate; polyhydric alcohols such as ethylene glycol, butylene glycol, propylene glycol, 1,3-butylene alcohol and glycerin. Ethers such as diethyl ether and petroleum ether; acetone, acetic acid and the like. Of these, lower alcohols are preferred, and ethanol is particularly preferred. These solvents can be used alone or in combination of two or more.

As the extraction method, a general method can be used, and examples thereof include a method of immersing the plant in an extraction solvent and a method of heating and refluxing. The obtained extract is used as it is or after the extract is concentrated or dried after solids are removed by filtration or centrifugation as necessary.
Moreover, the obtained extract can be used after further purification. For purification, a general method can be used, and examples thereof include adsorption / desorption using activated carbon, silica gel, a polymer carrier, column chromatography, liquid-liquid extraction, fractional precipitation, and the like.

In order to obtain a lipase activity inhibitor or blood triglyceride lowering agent, a pharmaceutically acceptable carrier, such as an excipient, a lubricant, a diluent, a binder, a disintegrant, an emulsifier, a stabilizer, a taste, as appropriate. It is preferable to use oral preparations such as tablets, capsules, granules, powders, syrups and the like; parenteral preparations such as injections and suppositories, using odorants.
The effective dose of the extract of the present invention is preferably 500 mg to 4,000 mg / day (adult).

The extract of the present invention may be blended in food and drink, and is particularly preferably a health food that promotes health. If it is blended in foods and drinks, it can be easily ingested, and can be used for the elimination / suppression / prevention of obesity and for the reduction of blood triglycerides.
In the present invention, the form of the food is not particularly limited, and examples thereof include drinks, granules, tablets, capsules, pastes and the like. Also, kamaboko, chikuwa and other kneaded products; bread and other fermented foods; milk products such as milk powder and fermented milk; butter and other fat and oil products; water, fruit juice, milk, soft drinks, soup and other beverages; added to confectionery and other foods Can also be used. Preservatives, colorants, sweeteners, antioxidants, thickening stabilizers, emulsifiers, seasonings, preservatives and other food additives, natural products, and the like can be used for such foods.
The extract of the present invention is preferably contained in a food or drink at a ratio of 1 to 95% by mass, particularly 5 to 90% by mass.

  Hereinafter, the present invention will be specifically described with reference to examples, but the present invention is not limited to these examples.

Examples 1-6
70 mL of ethanol was added to 10 g of each dry pulverized product of each plant leaf described in Table 1, and the mixture was refluxed for 2 hours. Subsequently, 60 mL of ethanol was added to the obtained residue, and extraction was repeated twice. The extract obtained in the first operation and the extract obtained in the second operation were combined and filtered again, and then the solvent was removed to obtain 1 to 1.8 g of each extract.

Example 7
0.8 g of an extract was obtained in the same manner as in Example 1 from 10 g of a dry pulverized bark of mud lilac (Glirichidia sepium (Jacq.) Walp).

Test example 1
A lipase activity inhibitory action confirmation test was conducted using each extract obtained in Examples 1 to 7 dissolved in dimethyl sulfoxide (DMSO).
The lipase activity inhibitory action was measured by using porcine pancreatic lipase (manufactured by Nacalai Tex Co., Ltd.), dissolved in 1.5 U / 30 mM Tris buffer, and subjected to each test. As the substrate, intralipos (1.2% egg yolk lecithin, 2.5% glycerol, 10% soybean oil; manufactured by Mitsubishi Pharma Corporation) was used.
In a mixed solution containing 25 μL of substrate, 150 μL of 30 mM Tris-HCl buffer (pH 8.5), 50 μL of 300 mM Tris-HCl buffer (pH 8.5), 50 μL of 1% cholic acid, 25 μL of 1 mM CaCl ₂ , the above Examples 1 to Each 2 μL of plant extract obtained in 7 was added and preheated at 37 ° C. for 30 minutes. Next, 200 μL of enzyme solution was added, and the mixture was further reacted at 37 ° C. for 30 minutes, and then a copper reagent (0.45 M triethanolamine, 0.05 M acetic acid, 3.4% copper sulfate pentahydrate, 20% sodium chloride). 1 mL was added to stop the reaction. To this, 3 mL of chloroform: n-heptane (4: 6) was added and centrifuged (3000 rpm, 7 minutes), and then a color former (0.1% bathocuproine, 0.05% butylhydroxyanisole / chloroform) was added to the supernatant. : 2 mL of n-heptane (4: 6)) was added, the absorbance of each sample was measured at a wavelength of 480 nm, and the generated free fatty acid was quantified. The extract of Adenanthera pavonina, Citrus hystrix, Michelia alba, Gustavia gracillima, Phyllanthus acidus and Thunbergia laurifolia has a final concentration of 25 μg / g. The extract of Glirichidia sepium (Jacq.) Walp was added at a final concentration of 10 μg / mL and 100 μg / mL. For the control, DMSO was added instead of the plant extract. To the blank, 30 mM Tris-HCl buffer was added instead of the enzyme.
The results are shown in Table 1 and FIG. The lipase activity inhibition value was expressed as a relative value of the amount of free fatty acid in each sample with the amount of free fatty acid in the control as 100%.

  As is clear from Table 1 and FIG. 1, all plant extracts inhibited pancreatic lipase activity in a concentration-dependent manner. In particular, in Bwaswan (Gustavia gracillima), Chiermai (Phyllanthus acidus), and Madol Lilac (Glirichidia sepium (Jacq.) Walp), the pancreatic lipase activity is suppressed to about 40% or less of the control in the presence of a final concentration of 100 μg / mL. It showed a remarkable inhibitory effect.

Test example 2
(1) Preparation of lipoprotein lipase The epididymal adipose tissue was excised from Wistar male rats (6-7 weeks of age), added with 30 mL Tris-HCl buffer (pH 8.5) 1 mL / 100 g adipose tissue, and hiscotron in ice. After crushing, the mixture was centrifuged (3000 rpm, 10 min, 4 ° C.) to remove the fat layer, and the supernatant was used as a crude enzyme preparation of lipoprotein lipase.
(2) Measurement of lipoprotein lipase activity The measurement of lipoprotein lipase uses intralipos (1.2% egg yolk lecithin, 2.5% glycerol, 10% soybean oil; manufactured by Mitsubishi Pharma Corporation) as a substrate. It was.
Fasting rat inactivated serum (heat treatment at 60 ° C., 10 minutes) of the same volume as 25 μL of the substrate was mixed and incubated at 37 ° C. for 30 minutes to obtain an activated substrate. 150 μL of 30 mM Tris-HCl buffer containing 2% bovine serum albumin was added to this activated substrate, and 2 μL of the extract obtained in Example 7 was further added, followed by addition of 200 μL of the crude enzyme solution at 37 ° C. The reaction was allowed for 30 minutes. The produced free fatty acid was quantified by a colorimetric method using Duncombe's method. The plant extract was added at a final concentration of 100 μg / mL. For the control, DMSO was added instead of the plant extract. Since lipoprotein lipase (LPL) activity was almost completely inhibited by 1M NaCl, lipase activities other than LPL were corrected.
The results are shown in Table 2.

  As apparent from Table 2, high lipoprotein lipase activity was observed in the plant extract of the present invention. Therefore, administration of the extract can reduce the blood triglyceride concentration, and when combined with the strong inhibitory action on the pancreatic lipase, it can be expected to improve hyperlipidemia along with obesity.

[Manufacture of food and drink]
Production Example 1 Supplement (Tablet Type)
Various ingredients were mixed and tableted according to the following formulation to obtain 3 types of supplements (weight per day; 4 tablets were eaten 3 times a day). In addition, the extract obtained by the method similar to the said Example 2, 5 and 7 was used as extract (1), respectively.

Extract (1) 2,400mg
Vitamin B2 3mg
Vitamin B6 3mg
Excipient 1,194mg
Total 3,600mg

Production Example 2 Beverages Various components were mixed according to the following formulation to obtain three types of beverages. In addition, the extract obtained by the method similar to the said Example 2, 5 and 7 was used as extract (1), respectively.

Extract (1) 1,000mg
Oligosaccharide 80mg
Aspartame 10mg
Fructose 1,700mg
Vitamin C 20mg
Citric acid appropriate amount (adjusted to pH 3.0-3.5)
Purified water
Total 100mL

Production Example 3 Soup 500 to 1,500 mg of the extract obtained in the same manner as in Examples 1 to 7 was added to commercially available soups to obtain 7 types of soups.

FIG. 1 is a diagram showing the results of measurement of lipase activity inhibitory action of plant extracts.

Claims (7)

  Mully lilac (Glirichidia sepium (Jacq.) Walp), Adenanthera pavonina, Citrus hystrix, Michelia alba, Gustavia gracillima, Phyllanthus lauri and hunter Or a lipase activity inhibiting food or drink comprising an extract of one or more plants selected from   The lipase activity inhibiting food or drink according to claim 1, wherein the plant extract is an extract obtained by extracting leaves or bark of a plant with a polar solvent.   A food or drink for lowering blood triglycerides, which contains an extract obtained by extracting bark of madir lilac (Glirichidia sepium (Jacq.) Walp) with a polar solvent.   Mully lilac (Glirichidia sepium (Jacq.) Walp), Adenanthera pavonina, Citrus hystrix, Michelia alba, Gustavia gracillima, Phyllanthus lauri and hunter A lipase activity inhibitor characterized by containing an extract of one or more plants selected from   The lipase activity inhibitor according to claim 4, wherein the plant extract is an extract obtained by extracting leaves or bark of a plant with a polar solvent.   The lipase activity inhibitor according to claim 5, wherein the polar solvent is ethanol.   A blood triglyceride-lowering agent characterized by comprising, as an active ingredient, an extract obtained by extracting bark of mud lilac (Glirichidia sepium (Jacq.) Walp) with a polar solvent.

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